Delving into the Latest Updates on Imidafenacin with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Imidafenacin (JAN/INN), KRP 197, KRP-197

+ [9]

Target

M1 receptor x M3 receptor

Mechanism

M1 receptor antagonists(Muscarinic acetylcholine receptor M1 antagonists), M3 receptor antagonists(Muscarinic acetylcholine receptor M3 antagonists)

Therapeutic Areas

Urogenital Diseases

Active Indication

Urinary Bladder, OveractivePollakisuriaUrinary Incontinence, Urge

Inactive Indication-

Originator Organization

KYORIN Pharmaceutical Co., Ltd.

Active Organization

Eisai Co., Ltd.R-Pharm Overseas, Inc.

Tianjin Hankang Pharmaceutical Biotechnology Co. Ltd.

+ [3]

Inactive Organization

R-Pharm JSC

Drug Highest PhaseApproved

First Approval Date

JP (18 Apr 2007),

Urinary Bladder, Overactive

Regulation-

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Structure

Molecular FormulaC20H21N3O

InChIKeySQKXYSGRELMAAU-UHFFFAOYSA-N

CAS Registry170105-16-5

主要目的：在空腹及餐后给药条件下，比较江苏联环药业股份有限公司提供的咪达那新片（规格：0.1 mg）与杏林製薬株式会社生产的咪达那新片（规格：0.1 mg，商品名：Uritos®）在健康成年人群中吸收程度和速度的差异，评价其生物等效性。次要目的：在空腹及餐后给药条件下，评价江苏联环药业股份有限公司提供的咪达那新片（规格：0.1 mg）的安全性。

[Translation]

Main purpose: To compare imidanacin tablets (specification: 0.1 mg) provided by Jiangsu Lihuan Pharmaceutical Co., Ltd. and imidanacin tablets (specification: 0.1 mg) produced by Xinglin Pharmaceutical Co., Ltd. under fasting and postprandial administration conditions. mg, trade name: Uritos®) in healthy adult populations to evaluate its bioequivalence. Secondary purpose: To evaluate the safety of midanacin tablets (specification: 0.1 mg) provided by Jiangsu Lihuan Pharmaceutical Co., Ltd. under fasting and postprandial administration conditions.

Start Date08 Aug 2024

Sponsor / Collaborator

Jiangsu Lianhuan Pharmaceutical Co., Ltd.

ChiCTR2300070562 / SuspendedNot ApplicableIIT

A randomized, open-label, two-formulation, two-period, crossover study of the bioequivalence of a single oral dose of Imidafenacin tablets in fasted and fed healthy Chinese subjects

Start Date17 Apr 2023

Sponsor / Collaborator-

CTR20202404 / CompletedNot Applicable

咪达那新片（0.1mg）在中国健康人群中空腹和餐后状态下单次给药的人体生物等效性临床试验

[Translation] A human bioequivalence clinical trial of imidacin tablets (0.1 mg) in Chinese healthy subjects after single administration in fasting and fed state

1. 以杏林制药株式会社生产的咪达那新片（0.1mg，商品名为URITOS）为参比制剂，以南京制药厂有限公司生产的咪达那新片（0.1mg）为受试制剂，通过单中心、随机、开放、单次给药、两制剂、两周期、两序列、交叉设计的临床试验来评价两种制剂在中国健康受试者中空腹和餐后状态下的生物等效性。 2. 观察受试制剂和参比制剂在中国健康受试者中的安全性。

[Translation]

1. Using imidafenacin tablets (0.1 mg, trade name Uritos) produced by Kyorin Pharmaceutical Co., Ltd. as the reference preparation and imidafenacin tablets (0.1 mg) produced by Nanjing Pharmaceutical Factory Co., Ltd. as the test preparation, a single-center, randomized, open, single-dose, two-preparation, two-cycle, two-sequence, crossover clinical trial was conducted to evaluate the bioequivalence of the two preparations in fasting and fed states in healthy Chinese subjects. 2. Observe the safety of the test preparation and the reference preparation in healthy Chinese subjects.

Start Date03 Dec 2020

Sponsor / Collaborator

Nanjing Pharmaceutical Factory

100 Clinical Results associated with Imidafenacin

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100 Translational Medicine associated with Imidafenacin

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100 Patents (Medical) associated with Imidafenacin

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106

Literatures (Medical) associated with Imidafenacin

19 Apr 2024·ACS chemical biology

Characterization of Chemical Interactions between Clinical Drugs and the Oral Bacterium, Corynebacterium matruchotii, via Bioactivity-HiTES

Article

Author: Kim, Jonghwan ; Kim, Chung Sub ; Kim, Ki Hyun ; Lee, Seoung Rak ; Song, Jeongwon ; Lee, Gyu Sung ; Lee, Bum Soo ; Park, Sehwan ; Lee, Da Yeong

In the field of natural product research, the rediscovery of already-known compounds is one of the significant issues hindering new drug development. Recently, an innovative approach called bioactivity-HiTES has been developed to overcome this limitation, and several new bioactive metabolites have been successfully characterized by this method. In this study, we applied bioactivity-HiTES to Corynebacterium matruchotii, the human oral bacterium, with 3120 clinical drugs as potential elicitors. As a result, we identified two cryptic metabolites, methylindole-3-acetate (MIAA) and indole-3-acetic acid (IAA), elicited by imidafenacin, a urinary antispasmodic drug approved by the Japanese Pharmaceuticals and Medical Devices Agency (PMDA). MIAA showed weak antibacterial activity against a pulmonary disease-causing Mycobacterium conceptionense with an IC₅₀ value of 185.7 μM. Unexpectedly, we also found that C. matruchotii metabolized fludarabine phosphate, a USFDA-approved anticancer drug, to 2-fluoroadenine which displayed moderate antibacterial activity against both Bacillus subtilis and Escherichia coli, with IC₅₀ values of 8.9 and 20.1 μM, respectively. Finally, acelarin, a prodrug of the anticancer drug gemcitabine, was found to exhibit unreported antibacterial activity against B. subtilis with an IC₅₀ value of 33.6 μM through the bioactivity-HiTES method as well. These results indicate that bioactivity-HiTES can also be applied to discover biotransformed products in addition to finding cryptic metabolites in microbes.

01 Jan 2024·Investigative and Clinical Urology

Efficacy and safety evaluation of imidafenacin administered twice daily for continency recovery following radical prostatectomy in prostate cancer patients: Prospective open-label case-controlled randomized trial

Article

Author: Kim, Soodong ; Goh, Hyeok Jun ; Lee, Kwang Min ; Lee, Jun Hee ; Choi, Dong Won ; Lee, Kisoo

PURPOSE:

This study aims to prospectively analyze the effects of anticholinergic therapy using imidafenacin on detrusor overactivity occurring after robot-assisted radical prostatectomy (RARP).

MATERIALS AND METHODS:

Patients were followed-up at outpatient visits 2-4 weeks post-surgery (visit 2) to confirm the presence of urinary incontinence. Those confirmed with urinary incontinence were randomly assigned in a 1:1 ratio to the anticholinergic medication group (imidafenacin 0.1 mg twice daily) or the control group. Patients were followed-up at 1, 3, and 6 months post-surgery for observational assessments, including the International Prostate Symptom Score (IPSS) and Overactive Bladder Symptom Score (OABSS).

RESULTS:

A total of 49 patients (25 in the treatment group and 24 in the control group) were randomized for the study. There were no differences observed between the groups in terms of age, comorbidities, prostate size, or pathological staging. According to the IPSS questionnaire results, there was no statistically significant difference between the medication and control groups (p=0.161). However, when comparing storage and voiding symptoms separately, there was a statistically significant improvement in storage symptom scores (p=0.012). OABSS also revealed statistically significant improvement in symptoms from 3 months post-surgery (p=0.005), which persisted until 6 months post-surgery (IPSS storage: p=0.023, OABSS: p=0.013).

CONCLUSIONS:

In the case of urinary incontinence that occurs after RARP, even if the function of the intrinsic sphincter is sufficiently preserved, if urinary incontinence persists due to changes in the bladder, pharmacological therapy using imidafenacin can be beneficial in managing urinary incontinence.

01 May 2023·Lower urinary tract symptoms

Efficacy and safety of vibegron compared with mirabegron for overactive bladder: A systematic review and network meta‐analysis

Review

Author: He, Wenjuan ; Zhang, Yuqian ; Sun, Qian ; Liu, Xiuju ; Huang, Guangliang ; Tian, Yunfei

Abstract:

Objectives:

The aim of this study was to indirectly compare the efficacy and safety of mirabegron and vibegron in patients with overactive bladder.

Methods:

A systematic search was performed on Pubmed, Web of Science, Embase, and the Cochrane Central Register of Controlled Trials databases to identify studies from the date of database inception to January 1, 2022. All randomized controlled trials comparing mirabegron or vibegron with tolterodine, imidafenacin, or placebo were eligible. One reviewer extracted data, and a second reviewer checked. Included trials were assessed for similarity, and networks were developed using Stata 16.0 software. Mean differences for continuous variables and odds ratios for dichotomous variables together with their 95% confidence intervals (CIs) were used to rank treatments and compare the differences, respectively.

Results:

A total of 11 randomized controlled trials and 10 806 patients were included. For each outcome, results for all licensed treatment doses were included. Both vibegron and mirabegron were more efficacious than placebo at reducing the frequency of micturition, incontinence, urgency, urgency incontinence, and nocturia. Vibegron was more efficacious than mirabegron in reducing mean voided volume/micturition (95% CI [5.15, 14.98]). Safety outcomes for vibegron and mirabegron were similar to those in the placebo group, except for mirabegron, which had a higher risk of nasopharyngitis and cardiovascular adverse events than placebo.

Conclusions:

Both drugs seem to be comparable and well tolerated, particularly as direct comparisons are not available. However, vibegron may be more effective than mirabegron in reducing mean voided volume.

100 Deals associated with Imidafenacin

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External Link

KEGG	Wiki	ATC	Drug Bank
D06273	Imidafenacin	G04BD	DB09262

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Urinary Bladder, Overactive	JP	KYORIN Pharmaceutical Co., Ltd.	18 Apr 2007
Urinary Bladder, Overactive	JP	Ono Pharmaceutical Co., Ltd.	18 Apr 2007

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Pollakisuria	NDA/BLA	RU	R-Pharm Overseas, Inc.	30 Jan 2022
Urinary Incontinence, Urge	Phase 1	CN	Tianjin Hankang Pharmaceutical Biotechnology Co. Ltd.	17 Jun 2015

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03575702 (Pubmed) Manual	Phase 3	Urinary Bladder, Overactive	300	imidafenacin	rjolkxmmus(qmkosfiwgf) = qcixaipqhn ixpgcasjuk (bgzvigvomx, 2.2) View more	Non-inferior	01 Jun 2019
				tolterodine	rjolkxmmus(qmkosfiwgf) = pittbylhsu ixpgcasjuk (bgzvigvomx, 1.8) View more
NCT03575702 (CTgov)	Phase 3	Urinary Bladder, Overactive	300	Uritos® (Uritos®)	jarursvrjl(frttqbmlqi) = gtpxujhvcr jsdbkfmppk (wiwgxvvmoo, zugnmxbdmz - ouwfpdwvgx) View more	-	21 May 2019
				Urotol® (Urotol®)	jarursvrjl(frttqbmlqi) = opsnosyzdu jsdbkfmppk (wiwgxvvmoo, clfolcqdow - hetullnbze) View more
NCT02294396 (CTgov)	Phase 4	Urinary Bladder, Overactive	649	Mirabegron tablet+Solifenacin tablet (Mirabegron + Solifenacin)	yzuovzvlol(ydymbwguxi) = iawhxnlvwf lgzzovzqpf (onragwobzv, jvuhkmwuch - raginsniac) View more	-	24 Dec 2018
				Mirabegron tablet+Propiverine tablet (Mirabegron + Propiverine)	yzuovzvlol(ydymbwguxi) = okxwjgvhvb lgzzovzqpf (onragwobzv, vuvcxghyec - wzbsbklwxm) View more
ADDITION STUDY (Pubmed \| Urology)	Not Applicable	Prostatic Hyperplasia \| Overactive bladder syndrome Add-on	308	Tamsulosin + Imidafenacin	dvfsabdewr(ddemlkkfls) = sgvzotfpei lisfcvfmwg (zgjxvbrzxx, 1.47 - 2.74) View more	Positive	01 Oct 2013